5α-Tetrahydrocorticosterone
5α-Tetrahydrocorticosterone (5α-HB), an endogenous steroid, is a glucocorticoid receptor (GR) agonist and a metabolite of Corticosterone (HY-B1618). 5α-Tetrahydrocorticosterone is an effective topical anti-inflammatory agent in vivo. 5α-Tetrahydrocorticosterone reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd of 268 nM. 5α-Tetrahydrocorticosterone can be used for research on inflammatory skin diseases.
For research use only. We do not sell to patients.
- CAS No.: 600-63-5
- Formula: C21H34O4
- Molecular Weight:350.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Endogenous Metabolite Isoforms
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Biological Activity
5α-Tetrahydrocorticosterone (0.001-100 μM) reduces metabolites that bind to GR-Corticosterone and its 5α-reduced metabolites in rat hepatocytes, with a Kd of 268 nM[1]. 5α-Tetrahydrocorticosterone (1 μM, 16 h) increases TAT and PEPCK mRNA in H4IIE cells[1]. 5α-Tetrahydrocorticosterone (1-10000 nM, 7 days) causes concentration-dependent suppression of vessel outgrowth from mouse aortic rings, with an EC50 of 2512 nM[2]. 5α-Tetrahydrocorticosterone (3 μM) increases the level of Mcp1 and Per1 and suppresses the expression of Pecam1 in aortic rings[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult lean male Zucker rats (6-8 weeks) were bilaterally adrenalectomized[1]
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Dosage:5 mg/kg
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Administration:i.p. for a single dose
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Result:Remained low plasma corticosterone levels.
Induced a classical negative feedback effect upon the hypothalamic-pituitary-adrenal axis.
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Animal Model:Male C57BL/6 mice with a single topical application of croton oil in ear skin[3]
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Dosage:25, 100, 200 μg
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Administration:Local administration for 28 days
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Result:Suppressed ear swelling in mice, with an ED50 of 23 μg.
Did not cause skin thinning, adrenal atrophy, weight loss, thymic involution, or raised insulin levels.
Chemical Information
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CAS No. 600-63-5
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Appearance Solid
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Molecular Weight 350.49
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Formula C21H34O4
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Color White to off-white
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SMILES
C[C@@]12[C@@H](C(CO)=O)CC[C@@]1([H])[C@]3([H])CC[C@@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])[C@@H](O)C2
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Synonyms
5α-THB
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. McInnes KJ, et al. 5alpha-reduced glucocorticoids, novel endogenous activators of the glucocorticoid receptor. J Biol Chem. 2004 May 28;279(22):22908-12. [Content Brief]
[2]. Abernethie AJ, et al. Comparison of mechanisms of angiostasis caused by the anti-inflammatory steroid 5α-tetrahydrocorticosterone versus conventional glucocorticoids. Eur J Pharmacol. 2022 Aug 15;929:175111. [Content Brief]
[3]. Livingstone DEW, et al. 5α-Tetrahydrocorticosterone: A topical anti-inflammatory glucocorticoid with an improved therapeutic index in a murine model of dermatitis. Br J Pharmacol. 2024 Apr;181(8):1256-1267. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)